Synthesis and preliminary biochemical evaluation of novel derivatives of PCP
(±)-Trans-Ph/Et and (±)-cis-Ph/Et 1-(2-ethyl-1- phenylcyclohexyl)piperidine were synthesized from 2-ethylcyclohexanone. In contrast to the corresponding trans-substituted 2-methyl compound which is 5x more potent than PCP, the trans-2-ethyl derivative has a 75x lower affinity for the PCP binding site. The cis-2-ethyl isomer is inactive like the cis-2-methyl derivative. (±)-1-(1-Phenylcyclohexyl)-2-methylpiperidine is almost as active as the parent PCP. Reduction of the aromatic ring or quaternization of the piperidine in PCP reduces the affinity for the PCP site.
Linders, Joannes T. M.,Furlano, David C.,Mattson, Mariena V.,Jacobson, Arthur E.,Rice, Kenner C.
experimental part
p. 79 - 87
(2011/01/13)
More Articles about upstream products of 7418-82-8